Azelastine

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Azelastine
Clinical data
Trade namesAstelin, Optivar, Allergodil, others.[1]
AHFS/Drugs.comMonograph
MedlinePlusa603009
License data
Pregnancy
category
  • AU: B3
Routes of
administration		Eye drops, nasal spray, by mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability40% (intranasal) [3]
Metabolitesdesmethylazelastine (active) [3]
Onset of actionWithin 1 hour [3]
Elimination half-life22 hours [3]
Duration of action12 hours [3]
Identifiers
  • (RS)-4-[(4-Chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-phthalazin-1-one
JSmol)
  • Clc1ccc(cc1)CC\3=N\N(C(=O)c2ccccc2/3)C4CCCN(C)CC4
  • InChI=1S/C22H24ClN3O/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16/h2-3,6-11,18H,4-5,12-15H2,1H3 checkY
  • Key:MBUVEWMHONZEQD-UHFFFAOYSA-N checkY
  (verify)

Azelastine, sold under the brand name Optivar among others, is a

skin rashes for which it is taken by mouth.[6] Onset of effects is within minutes when used in the eyes and within an hour when used in the nose.[7] Effects last for up to 12 hours.[7]

Common side effects include headache, sleepiness, change in taste, and sore throat.[7] It is unclear if use is safe during pregnancy or breastfeeding.[8] It is a second-generation antihistamine and works by blocking the release of a number of inflammatory mediators including histamine.[6][7]

Azelastine was patented in 1971 and came into medical use in 1986.

generic medication[2] in the United States. In 2021, it was the 145th most commonly prescribed medication in the United States, with more than 4 million prescriptions.[10][11]

Medical uses

Azelastine nasal spray is indicated for the local treatment of the symptoms of

vasomotor rhinitis in adults and children ≥ 12 years old.[14] Azelastine eye drops are indicated for the local treatment of seasonal and perennial allergic conjunctivitis.[15][16]

Side effects

Azelastine is safe and well tolerated in both adults and children with allergic rhinitis.[17][18][19] Bitter taste, headache, nasal burning and somnolence are the most frequently reported adverse events. US prescribing recommendations warn against the concurrent use of alcohol and/or other central nervous system depressants, but to date there have been no studies to assess the effects of azelastine nasal spray on the CNS in humans[needs update?]. More recent studies[20][21] have shown similar degrees of somnolence (approx. 2%) compared with placebo treatment.

The most common side effect is a bitter taste (about 20% of people). Due to this, the manufacturer has produced another formulation of azelastine with sucralose.[22] The problem of bitter taste may also be reduced by correct application of the nasal spray (i.e. slightly tipping the head forward and not inhaling the medication too deeply), or alternatively using the azelastine/sucralose formulation.[23]

In addition, anosmia (loss in the ability to smell) can occur with nasal spray antihistamines (including both formulations of azelastine).[7]

Pharmacology

Pharmacodynamics

Azelastine has a triple mode of action:[24]

  1. Anti-histamine effect,
  2. Mast-cell stabilizing effect and
  3. Anti-inflammatory effect.

Pharmacokinetics

The systemic

elimination half life, steady-state volume of distribution and plasma clearance are 22 h, 14.5 L/kg and 0.5 L/h/kg respectively (based on intravenous and oral administration data). Approximately 75% of an oral dose is excreted in feces. Pharmacokinetics of orally administered azelastine is not affected by age, gender, or hepatic impairment.[24]

Metabolism

Azelastine is oxidatively metabolized by the cytochrome P450 family into its active metabolite, desmethylazelastine, and two inactive carboxylic acid metabolites.[24]

Chemical properties

The chemical nomenclature of azelastine is (±)-1-(2H)-phthalazinone, 4-[(4-chlorophenyl) methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-monohydrochloride. It is white, almost odorless with a bitter taste.[25]

References

  1. ^ Drugs.com Drugs.com international listings for azelastine Page accessed 28 June 2015
  2. ^ a b "FDA Approves a Nasal Antihistamine for Nonprescription Use". U.S. Food and Drug Administration (FDA) (Press release). 17 June 2021. Retrieved 21 June 2021.
  3. ^
    ISBN 9780323044042
    . After intranasal administration, its systemic bioavailability is approximately 40%. Azelastine has an onset of action within the first hour of administration and reaches peak activity at 1–3 hours after administration. Duration of activity is about 12 hours. Intranasal administration results in maximal plasma concentrations in 2–3 hours. ... The half-life of the parent compound is 22 hours ...
  4. ISBN 9780857113382
    .
  5. S2CID 234142758
    . Intranasal H1 antihistamines such as azelastine are effective for controlling nasal symptoms. They need to be applied twice daily.
  6. ^
    ISBN 9780444537164
    .
  7. ^ a b c d e "Azelastine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists.
  8. ^ "Azelastine ophthalmic (Optivar) Use During Pregnancy". Drugs.com. Retrieved 26 March 2019.
  9. ISBN 9783527607495
    .
  10. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  11. ^ "Azelastine - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  12. ^ AHRQ Allergic Rhinitis and its Impact on Asthma (ARIA) treatment guidelines Archived 18 February 2013 at the Wayback Machine
  13. ^ "Rhinolast Nasal Spray Summary of Product Characteristics". October 2009. Retrieved 27 April 2010.
  14. ^ a b "Astelin- azelastine hydrochloride spray, metered".
  15. ^ "Optilast Eye Drops Summary of Product Characteristics". January 2010. Retrieved 27 April 2010.
  16. ^ "Optivar- azelastine hydrochloride solution/ drops".
  17. S2CID 46956783
    .
  18. PMID 7963150
    .
  19. PMID 8595539
    .
  20. PMID 15978303
    .
  21. PMID 17042145
    .
  22. S2CID 24449860
    .
  23. S2CID 25827650
    .
  24. ^
    S2CID 32512061
    .
  25. ^ drugs.com Azelastine Page accessed 28 June 2015
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